Pharmaceutical formulation for the active ingredient budesonide

Abstract

The invention relates to a pharmaceutical formulation containing essentially a) an inner layer which can optionally be applied to a core, with the active substance budesonide, bound with a binding agent; b) a middle layer with a polymer covering agent which is soluble in intestinal juice or retardant; and c) an outer envelope or outer layer which is resistant to stomach juice, said layers being able to contain in a manner known per se other pharmaceutically usual adjutants. The inventive formulation is characterised in that the binding agent is a polymer or a copolymer with acid groups and the formulation of the inner layer without the middle and outer layer releases the bound active ingredient in a release test according to USP XXIII monography <711> dissolution with apparatus 2 (addle) at a rotational speed of 100 / min in a phosphate buffer pH 7.5 after 30 min to a value of more than 80%.

Description

FIELD OF THE INVENTION [0001] The invention relates to a pharmaceutical formulation for the active ingredient budesonide PRIOR ART [0002] Löfberg, R. describes in “Research and Clinical Forums, Vol. 15 (5), pages 92-96 (1993), budesonide formulations for oral therapy of “inflammatory bowel desase (IBD)”. Described therein are budesonide pellets consisting of a sugar core with a thin budesonide layer in an undefined, water-insoluble rate limiting polymer and a coating of Eudragite® L 100-55. The pellets can be packed into gelatin capsules which represent the actual pharmaceutical form. [0003] WO 95 / 08323 describes budesonide pellets with controlled release profile and a process for producing them. To improve the solubility of budesonide, the active ingredient is applied to the pellet cores in a mixture of excipients. For this purpose, the active ingredient is suspended in an alcohol:water mixture of 0:100 to 20:80, and at least two parts of a suitable water-soluble excipient, e.g. α-...

AI Technical Summary

Benefits of technology

[0009] One object was regarded as being the provision of a budesonide formulation which avoids the prior art disadvantages. The production is intended to be possible entirely without the use of organic solvents. Excipients for increasing the solubility, like those mentioned in WO 95 / 08323, should be substantially avoided in order to reduce the risk of intolerance.

[0045] This can take place by simple crushing of extruded and cold pellets or hot cut.

Problems solved by technology

One problem with pharmaceutical formulations containing the active ingredient budesonide is the low solubility of the active ingredient.

This is regarded as disadvantageous because, at present, because of environmental and occupational safety considerations, avoidance of the use of organic solvents is always attempted.

In addition, the formulation must take place with water-soluble excipients, e.g. α-lactose monohydrate, sucrose or monosodium citrate, which may lead to unwanted side effects.